US5859031A - Small molecule inhibitors of rotamase enzyme activity - Google Patents

Small molecule inhibitors of rotamase enzyme activity Download PDF

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Publication number
US5859031A
US5859031A US08/650,461 US65046196A US5859031A US 5859031 A US5859031 A US 5859031A US 65046196 A US65046196 A US 65046196A US 5859031 A US5859031 A US 5859031A
Authority
US
United States
Prior art keywords
pyrrolidinecarboxylate
propyl
dimethyl
pyridyl
dioxopentyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
US08/650,461
Other languages
English (en)
Inventor
Gregory S. Hamilton
Joseph P. Steiner
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gliamed Inc
Original Assignee
GPI Nil Holdings Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US08/479,436 external-priority patent/US5614547A/en
Application filed by GPI Nil Holdings Inc filed Critical GPI Nil Holdings Inc
Priority to US08/650,461 priority Critical patent/US5859031A/en
Priority to SI9620091A priority patent/SI9620091B/sl
Priority to LU88833A priority patent/LU88833A1/de
Priority to CA002352900A priority patent/CA2352900A1/en
Priority to GB9817938A priority patent/GB2325230A/en
Priority to EP99126231A priority patent/EP0992492B1/en
Priority to GB9624257A priority patent/GB2305176B/en
Priority to NZ310292A priority patent/NZ310292A/en
Priority to HU0400694A priority patent/HUP0400694A3/hu
Priority to GB9815112A priority patent/GB2324527B/en
Priority to PCT/US1996/009701 priority patent/WO1996040633A1/en
Priority to JP50195897A priority patent/JP3561843B2/ja
Priority to CH02790/96A priority patent/CH688775A5/de
Priority to EEP200000317A priority patent/EE200000317A/xx
Priority to EA199700361A priority patent/EA002774B1/ru
Priority to SG9905533A priority patent/SG99293A1/en
Priority to IL13456296A priority patent/IL134562A/en
Priority to KR1020017007049A priority patent/KR100592604B1/ko
Priority to TR97/01504T priority patent/TR199701504T1/xx
Priority to IL12162196A priority patent/IL121621A0/xx
Priority to SG9906130A priority patent/SG94722A1/en
Priority to SG9906131A priority patent/SG94343A1/en
Priority to AU61062/96A priority patent/AU703118C/en
Priority to ES9950069A priority patent/ES2170628B1/es
Priority to SK1585-97A priority patent/SK158597A3/sk
Priority to CNB2004100019964A priority patent/CN1331853C/zh
Priority to CZ19972330A priority patent/CZ292529B6/cs
Priority to DE19680256T priority patent/DE19680256C2/de
Priority to GB9905606A priority patent/GB2332673A/en
Priority to CNB961945540A priority patent/CN1178912C/zh
Priority to EE9700335A priority patent/EE9700335A/xx
Priority to NZ510086A priority patent/NZ510086A/xx
Priority to EP96918384A priority patent/EP0769006B1/en
Priority to CZ2000315A priority patent/CZ295106B6/cs
Priority to ES009650030A priority patent/ES2131457B1/es
Priority to EP04007801A priority patent/EP1433781B1/en
Priority to PL96323300A priority patent/PL323300A1/xx
Priority to BR9608444A priority patent/BR9608444A/pt
Priority to IL13593796A priority patent/IL135937A0/xx
Priority to CA002206799A priority patent/CA2206799C/en
Priority to TW88118312A priority patent/TWI252226B/zh
Priority to TW85113067A priority patent/TW453992B/zh
Priority to ARP960104916A priority patent/AR004695A1/es
Priority to IDP963062A priority patent/ID16707A/id
Priority to ZA968983A priority patent/ZA968983B/xx
Priority to FI964328A priority patent/FI964328A/fi
Priority to SE9604098A priority patent/SE523522C2/sv
Priority to DK199601257A priority patent/DK176169B1/da
Assigned to GPI NIL HOLDINGS, INC. reassignment GPI NIL HOLDINGS, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: GUILFORD PHARMACEUTICALS INC.
Assigned to GPI NIL HOLDINGS, INC. reassignment GPI NIL HOLDINGS, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: GUILFORD PHARMACEUTICALS INC.
Priority to US08/787,161 priority patent/US5795908A/en
Priority to US08/833,629 priority patent/US6140357A/en
Priority to IL121621A priority patent/IL121621A/en
Priority to MXPA/A/1997/006714A priority patent/MXPA97006714A/xx
Priority to NO19974213A priority patent/NO317447B1/no
Priority to BG103977/99A priority patent/BG103977A/xx
Priority to BG102071A priority patent/BG102071A/xx
Priority to LVP-97-243A priority patent/LV11991B/en
Priority to HK98114580A priority patent/HK1013287A1/xx
Priority to HK00100914A priority patent/HK1022307A1/xx
Application granted granted Critical
Publication of US5859031A publication Critical patent/US5859031A/en
Priority to JP11043437A priority patent/JP2000204048A/ja
Priority to JP23572799A priority patent/JP4051651B2/ja
Priority to SE9903136A priority patent/SE527193C2/sv
Priority to DK199901519A priority patent/DK199901519A/da
Priority to IL13353399A priority patent/IL133533A0/xx
Priority to IL13456200A priority patent/IL134562A0/xx
Priority to RU2000105120/14A priority patent/RU2000105120A/ru
Priority to US09/605,475 priority patent/US6500959B1/en
Priority to AT14622000A priority patent/AT500193B1/de
Priority to AT14612000A priority patent/AT500192B1/de
Priority to GR20010400154T priority patent/GR3035326T3/el
Priority to ARP010104364A priority patent/AR030739A2/es
Priority to ARP010104365A priority patent/AR030740A2/es
Priority to US10/219,887 priority patent/US20040049046A1/en
Priority to NO20035643A priority patent/NO20035643D0/no
Priority to SE0400359A priority patent/SE0400359L/xx
Priority to HK05103704A priority patent/HK1071131A1/xx
Priority to US11/166,220 priority patent/US7282510B2/en
Assigned to GLIAMED, INC. reassignment GLIAMED, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: GPI IP, LLC, D/B/A MGL PHARMA
Priority to US11/871,358 priority patent/US7652060B2/en
Priority to US12/633,464 priority patent/US7960570B2/en
Priority to US13/111,543 priority patent/US20110218343A1/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/12—Oxygen or sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
US08/650,461 1995-06-07 1996-05-21 Small molecule inhibitors of rotamase enzyme activity Expired - Fee Related US5859031A (en)

Priority Applications (79)

Application Number Priority Date Filing Date Title
US08/650,461 US5859031A (en) 1995-06-07 1996-05-21 Small molecule inhibitors of rotamase enzyme activity
SI9620091A SI9620091B (sl) 1995-06-07 1996-06-05 Malomolekulski inhibitorji aktivnosti encima rotamaze
LU88833A LU88833A1 (de) 1995-06-07 1996-06-05 Kleine Inhibitor-Molekuele der Enzymaktivitaet von Rotamase
CA002352900A CA2352900A1 (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
GB9817938A GB2325230A (en) 1995-06-07 1996-06-05 Intermediate for Neurotrophic N-glyoxylprolyl esters
EP99126231A EP0992492B1 (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
GB9624257A GB2305176B (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
NZ310292A NZ310292A (en) 1995-06-07 1996-06-05 2-Acyl, N-substituted pyrrolidine derivative inhibitors of rotamase enzyme activity and their use in treating neurological disorders
HU0400694A HUP0400694A3 (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity and pharmaceutical compositions containing the compounds
GB9815112A GB2324527B (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
PCT/US1996/009701 WO1996040633A1 (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
JP50195897A JP3561843B2 (ja) 1995-06-07 1996-06-05 ロタマーゼ酵素活性の小分子阻害剤
CH02790/96A CH688775A5 (de) 1995-06-07 1996-06-05 Kleine Inhibitor-Molekuele der Enzymaktivitaet von Rotamase.
EEP200000317A EE200000317A (et) 1995-06-07 1996-06-05 Ühend, seda sisaldav farmatseutiline kompositsioon, keemiline ühend ja meetod nende valmistamiseks
EA199700361A EA002774B1 (ru) 1995-06-07 1996-06-05 Применение новых нейротрофных соединений для стимулирования роста и регенерации нейронов, для лечения неврологического расстройства и для предупреждения нейродегенерации и в приготовлении лекарственного средства
SG9905533A SG99293A1 (en) 1995-06-07 1996-06-05 Inhibitors of rotamase enzyme activity
IL13456296A IL134562A (en) 1995-06-07 1996-06-05 Pyrrolidine carboxylic acid derivatives and methods for their preparation
KR1020017007049A KR100592604B1 (ko) 1995-06-07 1996-06-05 로타마제 효소 활성의 소분자 억제제
TR97/01504T TR199701504T1 (xx) 1995-06-07 1996-06-05 Rotamaz enzim aktivitesinin k���k molek�ll� inhibit�rleri.
IL12162196A IL121621A0 (en) 1995-06-07 1996-06-05 Neurotrophic compounds pharmaceutical compositions containing them and their use
SG9906130A SG94722A1 (en) 1995-06-07 1996-06-05 Inhibitors of ratamaze enzyme activity
SG9906131A SG94343A1 (en) 1995-06-07 1996-06-05 Inhibitors of romatase enzyme activity
AU61062/96A AU703118C (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
ES9950069A ES2170628B1 (es) 1995-06-07 1996-06-05 Pequeños inhibidores de moleculas de la actividad de enzimas de rotamasa
SK1585-97A SK158597A3 (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
CNB2004100019964A CN1331853C (zh) 1995-06-07 1996-06-05 旋转异构酶活性的小分子抑制剂
CZ19972330A CZ292529B6 (cs) 1995-06-07 1996-06-05 Použití neurotropních sloučenin, jejich farmaceuticky přijatelných solí nebo hydrátů, jako nízkomolekulárních inhibitorů rotamázové aktivity enzymů
DE19680256T DE19680256C2 (de) 1995-06-07 1996-06-05 Verwendung kleiner Moleküle als Inhibitoren der Rotamase-Aktivität
GB9905606A GB2332673A (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
CNB961945540A CN1178912C (zh) 1995-06-07 1996-06-05 旋转异构酶活性的小分子抑制剂
EE9700335A EE9700335A (et) 1995-06-07 1996-06-05 Rotamaasse ensüümiaktiivsuse väikesemolekulilised inhibiitorid
NZ510086A NZ510086A (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity and their use in the treatment of neurological disorders
EP96918384A EP0769006B1 (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
CZ2000315A CZ295106B6 (cs) 1995-06-07 1996-06-05 Sloučenina, farmaceutická směs, obsahující tuto sloučeninu a způsob jejich přípravy
ES009650030A ES2131457B1 (es) 1995-06-07 1996-06-05 Pequeños inhibidores de moleculas de la actividad de enzimas de rotamasa.
EP04007801A EP1433781B1 (en) 1995-06-07 1996-06-05 Pyrrolidine carboxylic acid derivatives
PL96323300A PL323300A1 (en) 1995-06-07 1996-06-05 Low-molecule inhibitors of rotamase enzymatic activity
BR9608444A BR9608444A (pt) 1995-06-07 1996-06-05 Inibidores de molécula pequena de atividade de enzima rotamase
IL13593796A IL135937A0 (en) 1995-06-07 1996-06-05 The different uses of non-immunosuppressive compounds
CA002206799A CA2206799C (en) 1995-06-07 1996-06-05 Small molecule inhibitors of rotamase enzyme activity
TW88118312A TWI252226B (en) 1996-05-21 1996-10-24 Small molecule inhibitors of rotamase enzyme activity
TW85113067A TW453992B (en) 1996-05-21 1996-10-24 Small molecule inhibitors of rotamase enzyme activity
ARP960104916A AR004695A1 (es) 1996-05-21 1996-10-25 Compuestos y composiciones neurotroficos que tienen afinidad con las inmunofilinas del tipo fkbp, y aplicaciones de aquellas.
IDP963062A ID16707A (id) 1996-05-21 1996-10-25 Inhibitor aktivitas enzim rotamase berbentuk molekul kecil
ZA968983A ZA968983B (en) 1996-05-21 1996-10-25 Small molecule inhibitors of rotamase enzyme activity
FI964328A FI964328A (fi) 1995-06-07 1996-10-28 Rotamaasi-entsyymiaktiivisuuden pienimolekyyliset inhibiittorit
SE9604098A SE523522C2 (sv) 1995-06-07 1996-11-08 Inhibitorer av små molekyler med rotamasenzymaktivitet
DK199601257A DK176169B1 (da) 1995-06-07 1996-11-08 Anvendelse af ikke-immunosuppresiv neutrofisk forbindelse til fremstilling af medikament
US08/787,161 US5795908A (en) 1995-06-07 1997-01-23 Small molecule inhibitors of rotamase enzyme activity
US08/833,629 US6140357A (en) 1995-06-07 1997-04-08 Small molecule inhibitors of rotamase enzyme activity
IL121621A IL121621A (en) 1995-06-07 1997-08-26 Uses in the History of Pyrolidine Carboxylate for the Preparation of Pharmaceutical Preparations for the Treatment of Neurological Disorders
MXPA/A/1997/006714A MXPA97006714A (en) 1995-06-07 1997-09-03 Small molecula inhibitors of the activity of enzima rotam
NO19974213A NO317447B1 (no) 1995-06-07 1997-09-12 Sma-molekylaere inhibitorer av rotamase-enzym-aktivitet
BG102071A BG102071A (en) 1995-06-07 1997-11-27 Minor molecule inhibitors of rotamase enzymic activity
BG103977/99A BG103977A (en) 1995-06-07 1997-11-27 Low molecular rotamase enzymic activity inhibitors
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HK98114580A HK1013287A1 (en) 1995-06-07 1998-12-22 Small molecule inhibitors of rotamase enzyme activity
HK00100914A HK1022307A1 (en) 1995-06-07 1998-12-22 Small molecule inhibitors of rotamase enzyme activity
JP11043437A JP2000204048A (ja) 1995-06-07 1999-02-22 ロタマ―ゼ酵素活性の小分子阻害剤を含有する薬剤組成物
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SE9903136A SE527193C2 (sv) 1995-06-07 1999-09-06 Förfarande för framställning av 3-fenyl-1-propyl (2S)-1-(3,3-dimetyl- 1,2-dixopentyl)-2-pyrrolidinkarboxylat
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IL13353399A IL133533A0 (en) 1995-06-07 1999-12-15 Non-immunosuppressive compounds, process for their preparation and different uses thereof
IL13456200A IL134562A0 (en) 1995-06-07 2000-02-15 Use of non-immunosuppressive compounds for the preparation of pharmaceutical compositions
RU2000105120/14A RU2000105120A (ru) 1995-06-07 2000-03-02 Ингибиторы ферментативной активности ротамазы, являющиеся малыми молекулами
US09/605,475 US6500959B1 (en) 1995-06-07 2000-06-28 Pyrrolidine derivatives and processes for preparing same
AT14622000A AT500193B1 (de) 1995-06-07 2000-08-24 Neurotrophe verbindung und verfahren zu ihrer herstellung
AT14612000A AT500192B1 (de) 1995-06-07 2000-08-24 Neurotrophe verbindung, diese enthaltende pharmazeutische masse, verwendung der verbindung und verfahren zu ihrer herstellung
GR20010400154T GR3035326T3 (en) 1995-06-07 2001-01-31 Small molecule inhibitors of rotamase enzyme activity
ARP010104364A AR030739A2 (es) 1996-05-21 2001-09-14 Un compuesto no-inmunosupresivo derivado de la n-glioxilprolina, un metodo para prepararlo y composiciones farmaceuticas que lo comprenden
ARP010104365A AR030740A2 (es) 1996-05-21 2001-09-14 Un compuesto derivado de la n-glioxilprolina y un metodo para prepararlo
US10/219,887 US20040049046A1 (en) 1995-06-07 2002-08-16 Small molecule inhibitors of rotamase enzyme activity
NO20035643A NO20035643D0 (no) 1995-06-07 2003-12-17 Små molekyl¶re inhibitorer av rotamaseenzymaktivitet
SE0400359A SE0400359L (sv) 1995-06-07 2004-02-17 Inhibitorer av små molekyler med rotamasenzymaktivitet
HK05103704A HK1071131A1 (en) 1995-06-07 2005-04-30 Small molecule inhibitors of rotamase enzyme activity
US11/166,220 US7282510B2 (en) 1995-06-07 2005-06-27 Small molecule inhibitors of rotamase enzyme activity
US11/871,358 US7652060B2 (en) 1995-06-07 2007-10-12 Small molecule rotamase enzyme inhibitors
US12/633,464 US7960570B2 (en) 1995-06-07 2009-12-08 Small molecule inhibitors of rotamase enzyme activity
US13/111,543 US20110218343A1 (en) 1995-06-07 2011-05-19 Small molecule inhibitors of rotamase enzyme activity

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US08/479,436 US5614547A (en) 1995-06-07 1995-06-07 Small molecule inhibitors of rotamase enzyme
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US08/833,629 Expired - Fee Related US6140357A (en) 1995-06-07 1997-04-08 Small molecule inhibitors of rotamase enzyme activity
US09/605,475 Expired - Fee Related US6500959B1 (en) 1995-06-07 2000-06-28 Pyrrolidine derivatives and processes for preparing same
US10/219,887 Abandoned US20040049046A1 (en) 1995-06-07 2002-08-16 Small molecule inhibitors of rotamase enzyme activity
US11/166,220 Expired - Fee Related US7282510B2 (en) 1995-06-07 2005-06-27 Small molecule inhibitors of rotamase enzyme activity
US11/871,358 Expired - Fee Related US7652060B2 (en) 1995-06-07 2007-10-12 Small molecule rotamase enzyme inhibitors
US12/633,464 Expired - Fee Related US7960570B2 (en) 1995-06-07 2009-12-08 Small molecule inhibitors of rotamase enzyme activity
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US09/605,475 Expired - Fee Related US6500959B1 (en) 1995-06-07 2000-06-28 Pyrrolidine derivatives and processes for preparing same
US10/219,887 Abandoned US20040049046A1 (en) 1995-06-07 2002-08-16 Small molecule inhibitors of rotamase enzyme activity
US11/166,220 Expired - Fee Related US7282510B2 (en) 1995-06-07 2005-06-27 Small molecule inhibitors of rotamase enzyme activity
US11/871,358 Expired - Fee Related US7652060B2 (en) 1995-06-07 2007-10-12 Small molecule rotamase enzyme inhibitors
US12/633,464 Expired - Fee Related US7960570B2 (en) 1995-06-07 2009-12-08 Small molecule inhibitors of rotamase enzyme activity
US13/111,543 Abandoned US20110218343A1 (en) 1995-06-07 2011-05-19 Small molecule inhibitors of rotamase enzyme activity

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